Patents by Inventor Harald Rau

Harald Rau has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Hydrogel-Linked Prodrugs Releasing Tagged Drugs
    Publication number: 20160082123
    Abstract: The present invention relates to a process for the preparation of a hydrogel-linked prodrug releasing a tag moiety-biologically active moiety conjugate, to a hydrogel-linked prodrug releasing a tag moiety-bio logically active moiety conjugate obtainable by such process, to pharmaceutical compositions comprising said prodrug and their use as a medicament.
    Type: Application
    Filed: April 16, 2014
    Publication date: March 24, 2016
    Applicant: Ascendis Pharma A/S
    Inventors: Harald RAU, Nora KALUZA, Ulrich HERSEL, Thomas KNAPPE, Burkhardt LAUFER
  • Sterilization of biodegradable hydrogels
    Patent number: 9278139
    Abstract: The present invention relates to a terminal sterilization process for biodegradable PEG-based insoluble hydrogels using irradiation. The presence of a protective solvent ensures that the hydrogel remains intact with functionally preserved three-dimensional and physicochemical properties.
    Type: Grant
    Filed: January 26, 2015
    Date of Patent: March 8, 2016
    Assignee: Ascendis Pharma A/S
    Inventors: Harald Rau, Tobias Voigt, Ulrich Hersel
  • PEGylated recombinant human growth hormone compounds
    Patent number: 9272048
    Abstract: A chemically modified human Growth Hormone (rhGH) prepared by attaching a transient linker which comprises a polyethylene glycol. The chemically modified protein may have a much longer lasting rhGH activity than that of the unmodified rhGH, enabling reduced dose and scheduling opportunities and the modified rhGH may not cause lipoatrophy. Also includes methods of use for the treatment and/or prevention of diseases or disorders in which use of growth hormone is beneficial.
    Type: Grant
    Filed: April 29, 2009
    Date of Patent: March 1, 2016
    Assignee: Ascendis Pharma Growth Disorders Division A/S
    Inventors: Harald Rau, Susanne Kinderman, Torben Lebmann, Grethe Norskov Rasmussen, Ulrich Hersel, Thomas Wegge, Kennett Sprogoe
  • Long acting insulin composition
    Patent number: 9265723
    Abstract: The present invention relates to a pharmaceutical composition comprising an insulin compound in a concentration that is sufficient to maintain a therapeutically effective level of the insulin compound in blood plasma for at least 3 days characterized by having a pharmacokinetic profile in vivo with substantially no burst of the insulin compound. The present invention further relates to the use of an insulin compound for preparing said pharmaceutical composition as well as a kit of parts comprising said pharmaceutical composition.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: February 23, 2016
    Assignee: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Kennett Sprogoe, Felix Cleemann, Ulrich Hersel, Silvia Kaden-Vagt, Torben Lessmann, Harald Rau, Thomas Wegge
  • Polymeric prodrug with self-immolative linker
    Patent number: 9238686
    Abstract: A cascade carrier linked prodrug is described comprising a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier.
    Type: Grant
    Filed: February 5, 2013
    Date of Patent: January 19, 2016
    Assignee: Ascendis Pharma GmbH
    Inventors: Ulrich Hersel, Harald Rau, Robert Schnepf, Dirk Vetter, Thomas Wegge
  • Prodrugs containing an aromatic amine connected by an amido bond to a linker
    Patent number: 9173953
    Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein an aromatic amine containing biologically active moiety is connected (bound) by an amido bound to a linker. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: November 3, 2015
    Assignee: Ascendis Pharma AS
    Inventors: Harald Rau, Julia Baron, Ulrich Hersel, Mathias Krusch
  • Carrier-Linked Prostanoid Prodrugs
    Publication number: 20150306239
    Abstract: The present invention relates to carrier-linked prostanoid prodrugs of formula (I) Z1—(X0-L0-PG0)y (I), wherein Z1, X0, L0, PG0 and y have the meaning as indicated in the description and claims; pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising the same. It further relates to their use as medicaments, especially for treating, controlling, delaying or preventing pulmonary arterial hypertension.
    Type: Application
    Filed: December 6, 2013
    Publication date: October 29, 2015
    Applicant: ASCENDIS PHARMA A/S
    Inventors: Harald Rau, Guillaume Maitro, Ulrich Hersel, Oliver Keil, Thomas Wegge
  • VEGF Neutralizing Prodrugs for the Treatment of Ocular Conditions
    Publication number: 20150297740
    Abstract: The present invention relates to a pharmaceutical composition comprising one or more pharmaceutically acceptable excipient(s) and a VEGF neutralizing prodrug, which comprises a VEGF neutralizing biologically active moiety, for use in a method for the treatment of one or more ocular conditions.
    Type: Application
    Filed: October 8, 2013
    Publication date: October 22, 2015
    Inventors: Harald RAU, Thomas KNAPPE, Burkhardt Laufer, Romy REIMANN, Samuel WEISBROD, Kennett SPROGØE, Nicola BISEK, Sebastian STARK, Tobias VOIGT
  • DIAGNOSIS, PREVENTION AND TREATMENT OF DISEASES OF THE JOINT
    Publication number: 20150290337
    Abstract: The present invention relates to apolymeric prodrug for use in the treatment, prevention and/or diagnosis a disease of the joint and pharmaceutical compositions and medical devices comprising said polymeric prodrugs.
    Type: Application
    Filed: October 8, 2013
    Publication date: October 15, 2015
    Inventors: Dirk Vetter, Ulrich Hersel, Kennett Sprogøe, Nora Kaluza, Oliver Keil, Guillaume Maitro, Harald Rau
  • Prodrugs comprising an insulin linker conjugate
    Patent number: 9138462
    Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an insulin linker conjugate D-L1, wherein D is insulin; and -L1 is: wherein the dashed line indicates the attachment to one of the amino groups of the insulin by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by insulin.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: September 22, 2015
    Assignee: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Harald Rau, Felix Cleemann, Ulrich Hersel, Silvia Kaden-Vagt, Torben Lessman, Thomas Wegge
  • Hydrogel Prodrugs
    Publication number: 20150258205
    Abstract: The present invention relates to a process for the preparation of a hydrogel and to a hydrogel obtainable by said process. The present invention further relates to a process for the preparation of a hydrogel-spacer conjugate, to a hydrogel-spacer conjugate obtainable by said process, to a process for the preparation of a carrier-linked prodrug and to carrier-linked prodrugs obtainable by said process, in particular to carrier-linked prodrugs that provide for a controlled or sustained release of a drug from a carrier. In addition, the invention relates to the use of the hydrogel for the preparation of a carrier-linked prodrug.
    Type: Application
    Filed: October 8, 2013
    Publication date: September 17, 2015
    Inventors: Harald Rau, Tobias Voigt, Burkhardt Laufer, Nicola Bisek, Franziska Hahn, Thomas Knappe
  • PRODRUGS COMPRISING AN INSULIN LINKER CONJUGATE
    Publication number: 20150258207
    Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an insulin linker conjugate D-L, wherein D represents the insulin moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I), wherein the dashed line indicates the attachment to one of the amino groups of the insulin by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by insulin.
    Type: Application
    Filed: May 14, 2015
    Publication date: September 17, 2015
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Harald RAU, Felix CLEEMANN, Ulrich HERSEL, Silvia KADEN-VAGT, Torben LESSMANN, Thomas WEGGE
  • Prodrugs comprising an exendin linker conjugate
    Patent number: 9133276
    Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an exendin linker conjugate D-L1, wherein D represents an exendin moiety; and -L1 is represented by formula (I), wherein the dashed line indicates the attachment to one of the amino groups of the exendin moiety by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by exendin.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: September 15, 2015
    Assignee: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Felix Cleemann, Ulrich Hersel, Torben Lessman, Harald Rau
  • HYDROGEL FORMULATIONS
    Publication number: 20150238625
    Abstract: A polymeric prodrug composition including a hydrogel, a biologically active moiety and a reversible prodrug linker The prodrug linker covalently links the hydrogel and the biologically active moiety at a position and the hydrogel has a plurality of pores with openings on its surface. The diameter of the pores is larger than that of the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety.
    Type: Application
    Filed: May 8, 2015
    Publication date: August 27, 2015
    Applicant: ASCENDIS PHARMA A/S
    Inventors: Ulrich Hersel, Harald Rau, Robert Schnepf, Dirk Vetter, Thomas Wegge
  • DIPEPTIDE-BASED PRODRUG LINKERS FOR ALIPHATIC AMINE-CONTAINING DRUGS
    Publication number: 20150202317
    Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aliphatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
    Type: Application
    Filed: March 31, 2015
    Publication date: July 23, 2015
    Inventors: Harald Rau, Torben Leßmann
  • STERILIZATION OF BIODEGRADABLE HYDROGELS
    Publication number: 20150196667
    Abstract: The present invention relates to a terminal sterilization process for biodegradable PEG-based insoluble hydrogels using irradiation. The presence of a protective solvent ensures that the hydrogel remains intact with functionally preserved three-dimensional and physicochemical properties.
    Type: Application
    Filed: January 26, 2015
    Publication date: July 16, 2015
    Inventors: Harald Rau, Tobias Voigt, Ulrich Hersel
  • Dipeptide-based prodrug linkers for aliphatic amine-containing drugs
    Patent number: 9062094
    Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aliphatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: June 23, 2015
    Assignee: Ascendis Pharma AS
    Inventors: Harald Rau, Torben Lessmann
  • Hydrogel formulations
    Patent number: 9056126
    Abstract: A polymeric prodrug composition including a hydrogel, a biologically active moiety and a reversible prodrug linker. The prodrug linker covalently links the hydrogel and the biologically active moiety at a position and the hydrogel has a plurality of pores with openings on its surface. The diameter of the pores is larger than that of the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety.
    Type: Grant
    Filed: May 19, 2011
    Date of Patent: June 16, 2015
    Assignee: ASCENDIS PHARMA A/S
    Inventors: Ulrich Hersel, Harald Rau, Robert Schnepf, Dirk Vetter, Thomas Wegge
  • PRODRUGS OF HYDROXYL-COMPRISING DRUGS
    Publication number: 20150087688
    Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a biologically active moiety-linker conjugate D-L, wherein D is a hydroxyl-comprising biologically active moiety; and L is a promoiety comprising a moiety L1 represented by formula (I) and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer and Z is a carrier group. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
    Type: Application
    Filed: April 24, 2013
    Publication date: March 26, 2015
    Inventors: Ulrich Hersel, Torben Lebmann, Harald Rau
  • Sterilization of biodegradable hydrogels
    Patent number: 8986609
    Abstract: The present invention relates to a terminal sterilization process for biodegradable PEG-based insoluble hydrogels using irradiation. The presence of a protective solvent ensures that the hydrogel remains intact with functionally preserved three-dimensional and physicochemical properties.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: March 24, 2015
    Assignee: Ascendis Pharma A/S
    Inventors: Harald Rau, Tobias Voigt, Ulrich Hersel